Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘Merck & Co.’ Category


Posted by kinasepro on June 2, 2009

Two allosteric inhibitors are better then one!

AZD-6244 is Array’s MEK inhibitor [ARRY-886] which failed a solo ph2 endpoint not too long ago.

MK-2206 is Merck’s ph1 AKT inhibitor

Posted in Array, Astra, Merck & Co. | Leave a Comment »

Merck’s got Azaindoles

Posted by kinasepro on May 4, 2009



Posted in JAK, Merck & Co., PDK1 | Leave a Comment »

Banyu’s WEE1 candidate

Posted by kinasepro on November 7, 2008

Polymorph app: WO/2008/133866

Discovery app: WO/2006/126128


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Posted in Banyu, Merck & Co., Wee1 | 1 Comment »

VX-680, VX-667: Done

Posted by kinasepro on November 21, 2007

VX-680 halted as:

one patient experienced QTc prolongation.


and the follow-on, VX-667:

Failed to meet pharmacokinetic objectives in a Phase 1 trial

Posted in Aurora, Merck & Co., Vertex | 15 Comments »

PDB Update

Posted by kinasepro on October 30, 2007

Merck (WP) Chk1, 2R0U: BMCL

6-(3-aminopropyl)-4-(3-hydroxyphenyl)-9-(1H- pyrazol-4-yl)benzo[h]isoquinolin-1(2H)-one

Posted in Chk1, Merck & Co., PDB | 6 Comments »

IKK-b or Jak?

Posted by kinasepro on June 4, 2007

So Merck’s got WO/2007/061764 and the wordplay makes me think the bit about JAK is just a diversion and that the primary target is IKK-b.  You have to squint a little to see the similarity with the Millennium series, but as usual: what do I know.  Interesting series none-the-less.


Posted in IKK, JAK, Merck & Co. | Leave a Comment »


Posted by kinasepro on December 28, 2006

Merck MA‘s got Met


Posted in c-Met, Merck & Co. | Leave a Comment »


Posted by kinasepro on December 26, 2006

WO2006135604 is a recent Chk1 offering via Merck.


Posted in Chk1, Merck & Co. | Leave a Comment »


Posted by kinasepro on December 12, 2006

Oh wait I’m sorry Merck. My bad, I didn’t realize we’re calling it MK-0457 now. heh… Phase 1 update presented yesterday. The compound hits Aurora, JAK2, Abl etc. etc. and the current study is in ph1 for colorectal cancer. Looks good.

We’ve talked about the compound before here.

Posted in Aurora, clinical, Merck & Co., Vertex | Leave a Comment »


Posted by kinasepro on December 10, 2006

Ok Merck, so what’s with the aldehyde? Ahhah, I see you already dropped the dime in Biochemistry back in ’05. ‘Reductive amination’ with no reducing agent. Somebody needs to break these kinds of things down for me, since I still don’t get it.

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Posted in IGF, Merck & Co. | 2 Comments »